Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands

Abstract

Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R 3 -R 6 are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

What is claimed is:  
     
       1. A compound of the formula                    
       where G represents                    
       where 
       where Z is nitrogen, or methylene; and m is 1 or 2; and  
       R 3 , R 5 , and R 6  are the same or different and are selected from hydrogen, alkyl, —COR 11  or CO 2 R 11  where R 11  is alkyl or cycloalkyl having 3-7 carbon atoms; or —CONR 12 R 13  where R 12  and R 13  are selected independently from hydrogen, alkyl,  
       cycloalkyl having 3-7 carbon atoms, phenyl, 2-, 3-, or 4-pyridyl or NR 12 R 13  form a heterocyclic group which is morpholinyl, piperidinyl, pyrrolidinyl, or N-alkyl piperazinyl; or  
       R 5 -R 6  may be taken together to form a cyclic moiety having 3-7 carbon atoms; and  
       where each alkyl group forming an R 3  R 5 , or R 6  substituent or portion thereof may be substituted independently with hydroxy or mono- or dialkylamino where each alkyl is independently alkyl or cycloalkyl having 3-7 carbon atoms.  
     
     
       2. A compound according to  claim 1 , which is N-(2,3-Dihydro-1H-indol-6-yl)-4-oxo- 4,5,6,7-tetrahydro-1H-indole-3-carboxamide.